- Targeting PTEN using small molecule inhibitors.
Targeting PTEN using small molecule inhibitors.
Methods (San Diego, Calif.) (2015-03-10)
Lok Hang Mak, Rudiger Woscholski
PMID25747336
ABSTRACT
PTEN (phosphatase and tensin homologue deleted on chromosome 10) is well known as a tumour suppressor. It's PI(3,4,5)P3 lipid phosphatase activity is an important counteracting mechanism in PI 3-kinase (phosphoinositide 3-kinase) signalling. Furthermore, PTEN lies upstream of Akt kinase, a key enzyme in insulin signalling regulating glucose uptake and cell growth. Therefore, PTEN has recently gained attention as a valuable drug target for the treatment of diabetes, stroke, cardiac infarct and fertility. This review summarizes the use of small molecules as PTEN inhibitors. Currently available methodologies and techniques for accessing PTEN inhibition in vitro and in cellulo will be discussed.
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
Hydrochloric acid, meets analytical specification of Ph. Eur., BP, NF, fuming, 36.5-38%
Sigma-Aldrich
Dulbecco′s Modified Eagle′s Medium - low glucose, With 1000 mg/L glucose, L-glutamine, and sodium bicarbonate, liquid, sterile-filtered, suitable for cell culture
Sigma-Aldrich
Trypsin-EDTA solution, 10 ×, sterile-filtered, BioReagent, suitable for cell culture, 5.0 g porcine trypsin and 2 g EDTA, 4Na per liter of 0.9% sodium chloride
Sigma-Aldrich
Dulbecco′s Modified Eagle′s Medium - high glucose, With 4500 mg/L glucose and sodium bicarbonate, without L-glutamine and sodium pyruvate, liquid, sterile-filtered, suitable for cell culture, suitable for hybridoma
Sigma-Aldrich
Ammonium molybdate tetrahydrate, BioReagent, suitable for cell culture, suitable for insect cell culture, 81.0-83.0% MoO3 basis
Sigma-Aldrich
Chloroform, contains ethanol as stabilizer, meets analytical specification of BP, 99-99.4% (GC)
Supelco
Hydrogen chloride – methanol solution, ~1.25 m HCl (T), derivatization grade (GC derivatization), LiChropur™